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Description

A cell-permeable, allosteric Dynamin inhibitor (IC50 = 6.9 µ,M and 14 µ,M for full length Dynamin I and Dynamin II GTPase activity, respectively, in vitro). 10 µ,M of this compound results in cytokinesis failure at the abscission stage in HeLa cultures, with 82% of cells that enter into mitosis becoming multinucleated, and with 97% resulting in cell death. However, it displays a much reduced effect in NIH3T3 cells at the same concentration. It elicits a dose-dependent reduction in cell growth against SMA-560, SJ-G2, SW480, MCF-7 and A2780 cultures, as being the most sensitive among a panel of other cancer cell lines (GI50 = 4.0-37 µ,M). It was further shown to be 6-fold more active (IC50 = 5.0 µ,M) than dynamin mediated receptor mediated endocytosis (RME) in U2OS cells, and 15-fold more active (IC50 = 1.3 µ,M) than Dynasore (Cat. No. 324410) in another Dynamin I GTPase activity assay.